195436-65-8Relevant academic research and scientific papers
Palladium-Catalyzed Cross-Coupling of gem-Bis(boronates) with Aryl Halides: An Alternative to Access Quaternary α-Aryl Aldehydes
Zheng, Purui,Zhai, Yujie,Zhao, Xiaoming,Xu, Tao
supporting information, p. 393 - 396 (2019/01/23)
The compounds with a quaternary α-aryl aldehyde skeleton are important units in organic chemistry. Previously, the aryl group and carbonyl group are introduced in a stepwise manner. Herein, a novel route is developed to construct the quaternary α-aryl aldehydes with gem-bis(boronates) as precursors, in which the two groups are installed simultaneously. The gem-bis(boronates) are readily available from ketones; as a result, this methodology provides a more general strategy to produce the quaternary α-aryl aldehydes with broad scopes and synthetic convenience.
One-Pot Synthesis of Spirocyclic or Fused Pyrazoles from Cyclic Ketones: Calcium Carbide as the Carbon Source in Ring Expansion
Yu, Yue,Chen, Yang,Huang, Wei,Wu, Wanqing,Jiang, Huanfeng
, p. 9479 - 9486 (2017/09/23)
N-Tosylhydrazones generated in situ from cyclic ketones smoothly underwent a [3 + 2] cycloaddition to afford saturated spirocyclic pyrazoles and further transformed to the fused analogues via a ring expansion in certain cases. An inexpensive and renewable
Design and synthesis of novel small molecule CCR2 antagonists: Evaluation of 4-aminopiperidine derivatives
Vilums,Zweemer,Dekkers,Askar,De Vries,Saunders,Stamos,Brussee,Heitman,Ijzerman
supporting information, p. 5377 - 5380 (2015/01/09)
A novel N-(2-oxo-2-(piperidin-4-ylamino)ethyl)-3-(trifluoromethyl)benzamide series of human CCR2 chemokine receptor antagonists was identified. With a pharmacophore model based on known CCR2 antagonists a new core scaffold was designed, analogues of it synthesized and structure-affinity relationship studies derived yielding a new high affinity CCR2 antagonist N-(2-((1-(4-(3-methoxyphenyl)cyclohexyl)piperidin-4-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide.
